Application | Comment | Organism |
---|---|---|
medicine | by blocking isoform PDE5, vardenafil may be used in bladder dysfunction by ameliorating irritative lower urinary tract symptoms | Rattus norvegicus |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
Cilostamide | - |
Homo sapiens | |
Cilostamide | - |
Rattus norvegicus | |
dipyridamole | - |
Homo sapiens | |
dipyridamole | - |
Rattus norvegicus | |
sildenafil | blocking of 70% of total cGMP hydrolizing activity | Homo sapiens | |
sildenafil | blocking of 70% of total cGMP hydrolizing activity | Rattus norvegicus | |
tadalafil | blocking of 70% of total cGMP hydrolizing activity | Homo sapiens | |
tadalafil | blocking of 70% of total cGMP hydrolizing activity | Rattus norvegicus | |
vardenafil | blocking of 70% of total cGMP hydrolizing activity. Blocking of enzyme with vardenafil increases the antiproliferative and relaxant effect of sodium nitroprusside on cells, which is almost ineffective in presence of active enzyme | Homo sapiens | |
vardenafil | blocking of 70% of total cGMP hydrolizing activity. Blocking of enzyme with vardenafil increases the antiproliferative and relaxant effect of sodium nitroprusside on cells, which is almost ineffective in presence of active enzyme | Rattus norvegicus | |
zaprinast | - |
Homo sapiens | |
zaprinast | - |
Rattus norvegicus |
Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
---|---|---|---|---|---|---|
additional information | Rattus norvegicus | isoform PDE5 regulates bladder smooth muscle tone, strongly limiting the nitric oxide/cGMP signaling | ? | - |
? |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | - |
isoform PDE5 | - |
Rattus norvegicus | - |
isoform PDE5 | - |
Source Tissue | Comment | Organism | Textmining |
---|---|---|---|
bladder | vascular endothelium and muscle fibers | Homo sapiens | - |
bladder | vascular endothelium and muscle fibers, castration decreases and T supplementation restores PDE5 gene expression | Rattus norvegicus | - |
muscle | muscle fibers of bladder | Homo sapiens | - |
muscle | muscle fibers of bladder | Rattus norvegicus | - |
vascular endothelium | - |
Homo sapiens | - |
vascular endothelium | - |
Rattus norvegicus | - |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
additional information | isoform PDE5 regulates bladder smooth muscle tone, strongly limiting the nitric oxide/cGMP signaling | Rattus norvegicus | ? | - |
? |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
0.0000003 | - |
bladder homogenate, 30°C, pH 7.0 | Homo sapiens | vardenafil | |
0.0000032 | - |
bladder homogenate, 30°C, pH 7.0 | Homo sapiens | sildenafil | |
0.00000607 | - |
bladder homogenate, 30°C, pH 7.0 | Homo sapiens | tadalafil | |
0.0000088 | - |
bladder homogenate, 30°C, pH 7.0 | Homo sapiens | zaprinast | |
0.0000109 | - |
bladder homogenate, 30°C, pH 7.0 | Homo sapiens | dipyridamole | |
0.0000405 | - |
bladder homogenate, 30°C, pH 7.0 | Homo sapiens | Cilostamide |